Tityustoxin-K alpha, a structurally novel and highly potent K+ channel peptide toxin, interacts with the alpha-dendrotoxin binding site on the cloned Kv1.2 K+ channel.

abstract：:The synthetic alpha-conotoxin Vc1.1 is a small disulfide bonded peptide currently in development as a treatment for neuropathic pain. Unlike Vc1.1, the native post-translationally modified peptide vc1a does not act as an analgesic in vivo in rat models of neuropathic pain. It has recently been proposed that the primar...

journal_title：Molecular pharmacology

authors： Nevin ST,Clark RJ,Klimis H,Christie MJ,Craik DJ,Adams DJ

更新日期：2007-12-01 00:00:00

abstract：:The endogenous bronchodilator, S-nitrosoglutathione (GSNO), increases expression, maturation, and function of both the wild-type and the DeltaF508 mutant of the cystic fibrosis transmembrane conductance regulatory protein (CFTR). Though transcriptional mechanisms of action have been identified, GSNO seems also to have...

journal_title：Molecular pharmacology

authors： Zaman K,Carraro S,Doherty J,Henderson EM,Lendermon E,Liu L,Verghese G,Zigler M,Ross M,Park E,Palmer LA,Doctor A,Stamler JS,Gaston B

更新日期：2006-10-01 00:00:00

abstract：:Voltage-gated sodium channels are inhibited by many local anesthetics, antiarrhythmics, and antiepileptic drugs. The local anesthetic lidocaine appears to be able to access its binding site in the sodium channel only from the membrane phase or from the internal face of the channel. In contrast, the antiepileptic drug ...

journal_title：Molecular pharmacology

authors： Jo S,Bean BP

更新日期：2014-02-01 00:00:00

abstract：:The UGT1 locus is felt to be highly conserved between species, as is evident from the characterization of the locus in rodents and humans. In rabbits, cDNAs encoding proteins homologous to human UGT1A4, UGT1A6, and UGT1A7 have previously been identified. Here we demonstrate by Southern blot analysis, using exon 1 dive...

journal_title：Molecular pharmacology

authors： Li Q,Lamb G,Tukey RH

更新日期：2000-07-01 00:00:00

abstract：:Glucose utilization in isolated islets of Langerhans of the rat was determined by measuring the conversion of [5-3H]glucose (10 mM) to 3H2O. The alpha 2-adrenoceptor agonists clonidine, epinephrine, and norepinephrine in the presence of the alpha 1-adrenoceptor antagonist prazosin and the beta-adrenoceptor antagonist ...

journal_title：Molecular pharmacology

authors： Laychock SG

更新日期：1987-08-01 00:00:00

abstract：:Mouse embryonic spinal cord neurons in culture exhibit spontaneous calcium oscillations from day in vitro (DIV) 6 through DIV 10. Such spontaneous activity in developing spinal cord contributes to maturation of synapses and development of pattern-generating circuits. Here we demonstrate that these calcium oscillations...

journal_title：Molecular pharmacology

authors： Kelamangalath L,Dravid SM,George J,Aldrich JV,Murray TF

更新日期：2011-06-01 00:00:00

abstract：:Ceramides are naturally occurring compounds recognized to mediate apoptosis. N-acylsphingosines, containing a double bond at carbons 4 and 5 of their sphingoid backbone, are thought to be the active form, because N-acylsphinganines with completely saturated sphingoid are inactive. In the present study, we synthesized ...

journal_title：Molecular pharmacology

authors： Hwang O,Kim G,Jang YJ,Kim SW,Choi G,Choi HJ,Jeon SY,Lee DG,Lee JD

更新日期：2001-05-01 00:00:00

abstract：:Adenosine acting via A2a receptors (A2aR) is a potent cerebral vasodilator that relaxes vascular smooth muscle cells (VSMCs) by a mechanism attributed to activation of cAMP-dependent protein kinase (cAK). We examined effects of adenosine and its mechanism of action on L-type Ca2+ channels in native VSMCs from rat basi...

journal_title：Molecular pharmacology

authors： Murphy K,Gerzanich V,Zhou H,Ivanova S,Dong Y,Hoffman G,West GA,Winn HR,Simard JM

更新日期：2003-09-01 00:00:00

abstract：:Amphetamine congeners [e.g., 3,4-methylenedioxymetamphetamine (MDMA), or "ecstasy"] are substrates for monoamine transporters (i.e., the transporters for serotonin, norepinephrine, and dopamine); however, their in vivo-action relies on their ability to promote monoamine efflux. The mechanistic basis for this counter t...

journal_title：Molecular pharmacology

authors： Seidel S,Singer EA,Just H,Farhan H,Scholze P,Kudlacek O,Holy M,Koppatz K,Krivanek P,Freissmuth M,Sitte HH

更新日期：2005-01-01 00:00:00

abstract：:The immunosuppressive agent cyclosporine A has been shown to reverse multidrug resistance (MDR) in malignant cells. In the present study, a 3H-cyclosporine diazirine analogue was used to photolabel viable MDR Chinese hamster ovary cells. The 170-kDa membrane P-glycoprotein, which functions as a drug efflux pump, was s...

journal_title：Molecular pharmacology

authors： Foxwell BM,Mackie A,Ling V,Ryffel B

更新日期：1989-10-01 00:00:00

abstract：:Ligands that selectively inhibit human α3β2 and α6β2 nicotinic acetylcholine receptor (nAChRs) and not the closely related α3β4 and α6β4 subtypes are lacking. Current α-conotoxins (α-Ctxs) that discriminate among these nAChR subtypes in rat fail to discriminate among the human receptor homologs. In this study, we desc...

journal_title：Molecular pharmacology

authors： Hone AJ,McIntosh JM,Azam L,Lindstrom J,Lucero L,Whiteaker P,Passas J,Blázquez J,Albillos A

更新日期：2015-11-01 00:00:00

abstract：:We have synthesized and characterized a high-affinity alpha 1-adrenergic receptor probe, 4-amino-6,7-dimethoxy-2[4'- [5"(3"'-125I-iodo-4"'-aminophenyl)pentanoyl]-1'-piperazinyl] quinazoline (125I-A55453). This ligand binds reversibly to rat hepatic plasma membranes with high affinity (KD = 77 +/- 6 pM), and it labels ...

journal_title：Molecular pharmacology

authors： Dickinson KE,Leeb-Lundberg LM,Heald SL,Wikberg JE,DeBernardis JF,Caron MG,Lefkowitz RJ

更新日期：1984-09-01 00:00:00

abstract：:The current study was designed to investigate the importance of cationic amino acid transporters (CATs) for the L-arginine supply to nitric oxide (NO) synthases in mouse J774A.1 macrophages and human EA.hy926 endothelial cells. CAT-1 was expressed in both cell types, whereas CAT-2B was only expressed in activated macr...

journal_title：Molecular pharmacology

authors： Closs EI,Scheld JS,Sharafi M,Förstermann U

更新日期：2000-01-01 00:00:00

abstract：:One-electron oxidation of several derivatives of pyrazolin-5-one, including the drug antipyrine, were studied by pulse radiolysis of aqueous solutions. All the compounds were found to be oxidized by Br2 rapidly (k approximately 3 X 10(8)-2 X 10(9) M-1 s-1) but considerably more slowly by weaker oxidants, such as perox...

journal_title：Molecular pharmacology

authors： Jovanovic SV,Neta P,Simic MG

更新日期：1985-10-01 00:00:00

abstract：:Inflammation contributes to pain hypersensitivity through multiple mechanisms. Among the most well characterized of these is the sensitization of primary nociceptive neurons by arachidonic acid metabolites such as prostaglandins through G protein-coupled receptors. However, in light of the recent discovery that the no...

journal_title：Molecular pharmacology

authors： Taylor-Clark TE,Undem BJ,Macglashan DW Jr,Ghatta S,Carr MJ,McAlexander MA

更新日期：2008-02-01 00:00:00

abstract：:The precise mechanism by which the broad-spectrum anti-RNA virus agent ribavirin elicits its in vitro antiviral effect has remained a matter of debate. We have demonstrated that inhibition of cellular inosine monophosphate dehydrogenase (IMPDH) activity, and thus depletion of intracellular GTP pools, is the predominan...

journal_title：Molecular pharmacology

authors： Leyssen P,De Clercq E,Neyts J

更新日期：2006-04-01 00:00:00

abstract：:The blocking effects of guanethidine on electrically induced, neurally mediated, contractions of the guinea pig vas deferens in vitro could be markedly antagonized by the bee venom polypeptide apamin (20-60 nM), by 0.1 mM methylene blue, and (less regularly) by 0.1-0.15 mM quinine, three substances known to inhibit ca...

journal_title：Molecular pharmacology

authors： Stutzin A,Paravic F,Ormenño G,Orrego F

更新日期：1983-03-01 00:00:00

abstract：:Tumor necrosis factor α (TNFα) plays a vital role in cancer progression as it is associated with inflammation and promotion of cancer angiogenesis and metastasis. The effects of TNFα are mediated by its downstream target, the oncogene lysine-rich CEACAM1 coisolated protein (LYRIC, also known as metadherin or astrocyte...

journal_title：Molecular pharmacology

authors： Xi R,Pun IH,Menezes SV,Fouani L,Kalinowski DS,Huang ML,Zhang X,Richardson DR,Kovacevic Z

更新日期：2017-05-01 00:00:00

abstract：:Tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione (TIBO) derivatives (e.g., R82150) are potent, human immunodeficiency virus-1 (HIV-1)-specific, inhibitors of reverse transcriptase (RT) that are undergoing initial evaluation in clinical trials. Because HIV-1 has become resistant to other RT inhibitor...

journal_title：Molecular pharmacology

authors： Mellors JW,Im GJ,Tramontano E,Winkler SR,Medina DJ,Dutschman GE,Bazmi HZ,Piras G,Gonzalez CJ,Cheng YC

更新日期：1993-01-01 00:00:00

abstract：:The class III antiarrhythmic drugs amiodarone and bretylium tosylate are cationic/amphiphilic, and various substances with these physico-chemical properties are known to directly activate heterotrimeric regulatory G proteins. We asked the question of whether class III antiarrhythmic drugs are also direct G protein act...

journal_title：Molecular pharmacology

authors： Hagelüken A,Nürnberg B,Harhammer R,Grünbaum L,Schunack W,Seifert R

更新日期：1995-02-01 00:00:00

abstract：:Guinea pig lung microsomes converted arachidonic acid (AA) to two classes of cytochrome P450 (P450)-dependent metabolites, 16- through 20-hydroxyeicosatetraenoic acids [(16-20)-OH-AA] and epoxyeicosatrienoic acids (EETs). The rate of formation of (16-20)-OH-AA was approximately 3-fold higher in microsomes from beta-na...

journal_title：Molecular pharmacology

authors： Knickle LC,Bend JR

更新日期：1994-06-01 00:00:00

abstract：:Bupropion is an atypical antidepressant that also has usefulness as a smoking-cessation aid. Because hydroxybupropion, a major metabolite of bupropion, is believed to contribute to its antidepressant activity, this metabolite may also contribute to the smoking-cessation properties of bupropion. This study investigated...

journal_title：Molecular pharmacology

authors： Damaj MI,Carroll FI,Eaton JB,Navarro HA,Blough BE,Mirza S,Lukas RJ,Martin BR

更新日期：2004-09-01 00:00:00

abstract：:Trypanosoma brucei encodes a relatively high number of genes of the equilibrative nucleoside transporter (ENT) family. We report here the cloning and in-depth characterization of one T. brucei brucei ENT member, TbNT9/AT-D. This transporter was expressed in Saccharomyces cerevisiae and displayed a uniquely high affini...

journal_title：Molecular pharmacology

authors： Al-Salabi MI,Wallace LJ,Lüscher A,Mäser P,Candlish D,Rodenko B,Gould MK,Jabeen I,Ajith SN,de Koning HP

更新日期：2007-03-01 00:00:00

abstract：:Computer simulations on a new model of the alpha1b-adrenergic receptor based on the crystal structure of rhodopsin have been combined with experimental mutagenesis to investigate the role of residues in the cytosolic half of helix 6 in receptor activation. Our results support the hypothesis that a salt bridge between ...

journal_title：Molecular pharmacology

authors： Greasley PJ,Fanelli F,Rossier O,Abuin L,Cotecchia S

更新日期：2002-05-01 00:00:00

abstract：:Tritiated dextromethorphan ([3H]DM) binds to two distinct sites in guinea pig brain, a high-affinity site (Kd = 13-20 nM) and a low-affinity site (Kd greater than 200 nM). Binding of [3H] DM to the high-affinity site is rapid, reversible, saturable, proportional to tissue concentration, and pH-dependent. The sites hav...

journal_title：Molecular pharmacology

authors： Craviso GL,Musacchio JM

更新日期：1983-05-01 00:00:00

abstract：:Inhibitors of the serotonin transporter (SERT) are widely used antidepressant agents, but the structural mechanism for inhibitory activity and selectivity over the closely related norepinephrine transporter (NET) is not well understood. Here we use a combination of chemical, biological, and computational methods to de...

journal_title：Molecular pharmacology

authors： Andersen J,Stuhr-Hansen N,Zachariassen LG,Koldsø H,Schiøtt B,Strømgaard K,Kristensen AS

更新日期：2014-05-01 00:00:00

abstract：:Celecoxib (CE) is a nonsteroidal anti-inflammatory drug (NSAID) that is a specific inhibitor of cyclooxygenase 2 (COX2). It is indicated for a variety of chronic inflammatory conditions, including rheumatoid arthritis. Over the last few years, adverse cardiovascular effects and increased risk for heart attacks have be...

journal_title：Molecular pharmacology

authors： Alloza I,Baxter A,Chen Q,Matthiesen R,Vandenbroeck K

更新日期：2006-05-01 00:00:00

abstract：:Thiourea, phenylthiourea, and methimazole perfused into rat liver stimulated the biliary efflux of GSSG without affecting the excretion of GSH into either the bile or the caval perfusate. The thiocarbamide moiety appears essential, since perfusion with urea, phenylurea, or N-methylimidazole did not stimulate GSSG rele...

journal_title：Molecular pharmacology

authors： Krieter PA,Ziegler DM,Hill KE,Burk RF

更新日期：1984-07-01 00:00:00

abstract：:Undesired block of human ERG1 potassium channels is the basis for cardiac side effects of many different types of drugs. Therefore, it is important to know exactly why some drugs particularly bind to these channels with high affinity. Upon expression in mammalian cells and Xenopus laevis oocytes, we investigated the i...

journal_title：Molecular pharmacology

authors： Gessner G,Zacharias M,Bechstedt S,Schönherr R,Heinemann SH

更新日期：2004-05-01 00:00:00

abstract：:We describe here an approach to characterize various lesions induced in DNA by drug treatments, using three parameters: (a) release of single-stranded DNA fragments by cell lysis in dilute alkali, which result from enzymatic strand scission during DNA repair or chemical alterations of DNA; (b) the presence of high mol...

journal_title：Molecular pharmacology

authors： Lönn U,Lönn S

更新日期：1987-07-01 00:00:00